摘要
表没食子儿茶素没食子酸酯(EGCG)在辅助低分子量阳离子聚合物递送siRNA的过程中表现优异,但其本身是一个结构较为复杂的植物多酚基元,可以进一步拆分为表没食子儿茶素(EGC)和没食子酸(GA)2种多酚基元.而这2种基元分子同样具有抑制癌细胞、杀伤肿瘤细胞以及通过氢键和疏水相互作用力来结合蛋白质或核酸的能力.本文拟探究各类植物多酚基元EGCG,EGC和GA结合核酸的能力和分别在辅助低分子量阳离子聚合物递送siRNA的过程中起到的作用.实验结果表明,EGC辅助ε-聚赖氨酸(PLL)递送siRNA的效率仅次于EGCG,而通过增加EGC的用量可以达到与EGCG接近的递送效果.
Epigallocatechin gallate(EGCG)has demonstrated promising effects in promoting the delivery of siRNA by low molecular weight cationic polymers.EGCG can be further hydrolyzed into(-)-epigallocatechin(EGC)and gallic acid(GA)motifs.EGC and GA also have the effect of inhibiting cancer cells,killing tumor cells,and binding proteins or nucleic acids through the combination of hydrogen bonding and hydrophobic interactions.Herein,this study strives to perform a structure-function relationship investigation of plant polyphenol motifs(EGCG,EGC,and GA)in facilitation of condensation and delivery of siRNA by low molecular weight cationic polymers.It was found that EGCG exhibited the highest efficiency in promoting PLL-mediated siRNA delivery while EGC also showed a promising result,and the latter efficiency can be further improved by tailoring the dose of EGC in the complex.
作者
沈扬
朱方
沈湾湾
范倩倩
李乙文
程义云
SHEN Yang;ZHU Fang;SHEN Wanwan;FAN Qianqian;LI Yiwen;CHENG Yiyun(Shanghai Key Laboratory of Regulatory Biology,School of Life Sciences,East China Normal University,Shanghai 200241,China;College of Polymer Science and Engineering,State Key Laboratory of Polymer Materials Engineering,Sichuan University,Chengdu 610065,China;School of Molecular Science and Engineering,South China Advanced Institute for Soft Matter Science and Technology,South China University of Technology,Guangzhou 510640,China)
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2020年第4期633-638,共6页
Chemical Journal of Chinese Universities
基金
国家自然科学基金(批准号:21725402,21774079)
上海市科委基金(批准号:17XD1401600)资助.
作者简介
联系人:程义云,男,博士,研究员,博士生导师,主要从事生物大分子胞内递送相关的高分子材料研究.E-mail:yycheng@mail.ustc.edu.cn;李乙文,男,博士,研究员,博士生导师,主要从事多酚材料化学研究.E-mail:ywli@scu.edu.cn。